MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a K i value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent.
性状
Solid
IC50 & Target[1][2]
mAChR4
体外研究(In Vitro)
MK-6884 (compound 13; 0-22 μM) is a PAM of ACh function in a cell-based Ca mobilization assay, with an EC50 of 27 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
[C]MK-6884 (compound 13) shows non-displaceable binding potential (BP ND ) of 0.83 in rhesus monkeys.
[C]MK-6884 (approximately 185 MBq, <2 μg; single intravenous) distributes on the known presence of M4 receptors in the rhesus monkeys brain.
[C]MK-688 can penetrate the blood-brain barrier in monkeys. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Tong L, et al. Discovery of [C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases. J Med Chem. 2020;63(5):2411-2425.
溶解度数据
In Vitro: THF : 3.33 mg/mL (8.09 mM; Need ultrasonic)配制储备液